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Publications

Structural Insights into Interaction Mechanisms of Alternative Piperazine-urea YEATS Domain Binders in MLLT1

Ni X. et al, (2019), ACS Medicinal Chemistry Letters, 10, 1661 - 1666

A chemical toolbox for the study of bromodomains and epigenetic signaling

Wu Q. et al, (2019), Nature Communications, 10

ALK2 inhibitors display beneficial effects in preclinical models of ACVR1 mutant diffuse intrinsic pontine glioma

Carvalho D. et al, (2019), Communications Biology, 2

A Chemical Probe for Tudor Domain Protein Spindlin1 to Investigate Chromatin Function

Fagan V. et al, (2019), Journal of Medicinal Chemistry

C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays.

Le Bihan Y-V. et al, (2019), Eur J Med Chem, 177, 316 - 337

Discovery of a Potent and Selective Fragment-like Inhibitor of Methyllysine Reader Protein Spindlin 1 (SPIN1)

Xiong Y. et al, (2019), Journal of Medicinal Chemistry

A genetics-led approach defines the drug target landscape of 30 immune-related traits

Fang H. et al, (2019), Nature Genetics, 51, 1082 - 1091

Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening

Resnick E. et al, (2019), Journal of the American Chemical Society, 141, 8951 - 8968

ALK2 inhibitors display beneficial effects in preclinical models of ACVR1 mutant diffuse intrinsic pontine glioma.

Carvalho D. et al, (2019), Commun Biol, 2

Discovery of Pyrrolo[3,2-d]pyrimidin-4-one Derivatives as a New Class of Potent and Cell-Active Inhibitors of P300/CBP-Associated Factor Bromodomain

Huang L. et al, (2019), Journal of Medicinal Chemistry, 62, 4526 - 4542

Targeting the Small GTPase Superfamily through their Regulatory Proteins

Gray JL. et al, (2019), Angewandte Chemie International Edition

An Activity-Based Probe Targeting Non-Catalytic, Highly Conserved Amino Acid Residues within Bromodomains

D'Ascenzio M. et al, (2019), Angewandte Chemie International Edition, 58, 1007 - 1012

Design, Synthesis and Characterization of Covalent KDM5 Inhibitors

Vazquez-Rodriguez S. et al, (2019), Angewandte Chemie International Edition, 58, 515 - 519

Synthesis and Biological Investigation of (+)-JD1, an Organometallic BET Bromodomain Inhibitor

Hassell-Hart S. et al, (2019), Organometallics

Structure-Based Approach toward Identification of Inhibitory Fragments for Eleven-Nineteen-Leukemia Protein (ENL)

Heidenreich D. et al, (2018), Journal of Medicinal Chemistry, 61, 10929 - 10934

Discovery of an MLLT1/3 YEATS Domain Chemical Probe

Moustakim M. et al, (2018), Angewandte Chemie International Edition, 57, 16302 - 16307

Bench-Stable Transfer Reagent Facilitates the Generation of Trifluoromethyl-sulfonimidamides

Wright M. et al, (2018), The Journal of Organic Chemistry, 83, 9510 - 9516

Discovery of a novel allosteric inhibitor scaffold for polyadenosine-diphosphate-ribose polymerase 14 (PARP14) macrodomain 2

Moustakim M. et al, (2018), Bioorganic & Medicinal Chemistry, 26, 2965 - 2972

Halogen-Aromatic π Interactions Modulate Inhibitor Residence Times

Heroven C. et al, (2018), Angewandte Chemie International Edition, 57, 7220 - 7224

Identifying Small-Molecule Binding Sites for Epigenetic Proteins at Domain-Domain Interfaces

Bowkett D. et al, (2018), ChemMedChem, 13, 1051 - 1057

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